US5213802A
Expired / Lapsed
US
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Pharmaceutical formulations employing esterified alkoxylated polyols as vehicles
Assignee: Lyondell Chemical Technology LP
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Filing: 1990-09-24
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Granted: 1993-05-25
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Expires: 2010-09-24
Abstract
Abstract Pharmaceutical formulations employing novel non-allergenic, non-irritating, non-toxic, and non-digestible carriers, bases, or vehicles for topical or ingestible drug delivery are disclosed. The carriers are esterified alkoxylated polyols; preferred carrier embodiments include propoxylated glycerols which are esterified with C 8 -C 24 fatty acids. The non-digestibility of the esterified alkoxylated polyols permits, for example, delivery of medicaments taken orally directly to the lower gastrointestinal tract.
Inventors
- 👤 Lawrence W. Masten
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 16:28
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/06; A61K47/08; A61K47/14; A61K9/00; A61K9/0012; A61K9/0014
Claims Analysis
Total Claims: 28
Claim 1
Independent Claim
203 words
An improved pharmaceutical formulation comprising an effective amount of a medication ingredient in admixture with an esterified alkoxylated polyol carrier of formula ##STR18## wherein (a) P is an organic radical derived from a polyol, the sum of w+x+y+z is from 2 to 8, ##EQU5## is an average number in the range of from 0 to about 0.15, z is an average number in the range of from about 2 to the sum of w +x+y+z, A is an oxyalkylene unit having at least 3 carbon atoms, B is a C 7 14 C 23 hydrocarbon group, at least one of R 1 , R 2 , R 3 , or R 4 is a moiety other than hydrogen, and C 2 is a carbon that on average is from 0 to about 15 percent primary; (b) said values of m, n, w, x, y, and z are selected to provide suitable pharmaceutical carrier properties; (c) said esterified alkoxylated polyol carrier is present in an amount sufficient to impart suitable body or coverage to said formulation; (d) said esterified alkoxylated polyol carrier is substantially dermally non-allergenic, non-irritating, and non-digestible, and non-toxic; and (e) said pharmaceutical formulation is characterized by the absence of a foodstuff.
Claim 2
Dependent Claim
203 words
An improved pharmaceutical formulation comprising an effective amount of a medication ingredient in admixture with an esterified alkoxylated polyol carrier of formula ##STR18## wherein (a) P is an organic radical derived from a polyol, the sum of w+x+y+z is from 2 to 8, ##EQU5## is an average number in the range of from 0 to about 0.15, z is an average number in the range of from about 2 to the sum of w +x+y+z, A is an oxyalkylene unit having at least 3 carbon atoms, B is a C 7 14 C 23 hydrocarbon group, at least one of R 1 , R 2 , R 3 , or R 4 is a moiety other than hydrogen, and C 2 is a carbon that on average is from 0 to about 15 percent primary; (b) said values of m, n, w, x, y, and z are selected to provide suitable pharmaceutical carrier properties; (c) said esterified alkoxylated polyol carrier is present in an amount sufficient to impart suitable body or coverage to said formulation; (d) said esterified alkoxylated polyol carrier is substantially dermally non-allergenic, non-irritating, and non-digestible, and non-toxic; and (e) said pharmaceutical formulation is characterized by the absence of a foodstuff.
Claim 3
Dependent Claim
27 words
The pharmaceutical formulation of claim 1 wherein the esterified alkoxylated polyol carrier has an average value of [(m·z)+(n·y)] in the range of from 0 to about 15.
Claim 4
Dependent Claim
36 words
The pharmaceutical formulation of claim 1 wherein the P organic radical of the esterified alkoxylated polyol is derived from a polyol selected from the group consisting of diols, triols, tetrols, saccharides, sugar alcohols, and mixtures thereof.
Claim 5
Dependent Claim
35 words
The pharmaceutical formulation of claim 1 wherein the P organic radical of the esterified alkoxylated polyol is derived from a triol selected from the group consisting of glycerin, trimethylol propane, trihydroxyhexane, trihydroxypentane, and mixtures thereof.
Claim 6
Dependent Claim
40 words
The pharmaceutical formulation of claim 1 wherein the P organic radical of the esterified alkoxylated polyol carrier is derived from a saccharide selected from the group consisting of glucose, fructose, mannose, galactose, arabinose, xylose, sorbitol, sorbose, sucrose, and mixtures thereof.
Claim 7
Dependent Claim
33 words
The pharmaceutical formulation of claim 1 wherein the P organic radical of the esterified alkoxylated polyol is derived from a sugar alcohol of formula HOCH 2 (CHOH) n CH 2 OH, where n=2-6.
Claim 8
Dependent Claim
65 words
The pharmaceutical formulation of claim 1 wherein the ##STR19## group of the esterified alkoxylated polyol carrier is derived from a fatty acid selected from the group consisting of caprylic acid, capric acid, lauric acid, myristic acid, myristoleic acid, stearic acid, palmitic acid, palmitoleic acid, ricinoleic acid, linoleic acid, linolenic acid, elaeostearic acid, arachidic acid, behenic acid, erucic acid, oleic acid, heptadecanoic acid, and mixtures thereof.
Claim 9
Dependent Claim
27 words
The pharmaceutical formulation of claim 1 wherein the esterified alkoxylated polyol carrier has an average value of ##EQU6## in the range of from 0 to about 0.05.
Claim 10
Dependent Claim
21 words
The pharmaceutical formulation of claim 1 wherein B in the esterified alkoxylated polyol is a C 13 -C 21 hydrocarbon group.
Claim 11
Dependent Claim
57 words
The pharmaceutical formulation of claim 1 wherein A in the esterified alkoxylated polyol is an oxyalkylene group derived from an epoxide selected from the group consisting of propylene oxide, 1,2-butylene oxide, isobutylene oxide, 2,3-butylene oxide, epichlorohydrin, allyl glycidyl ether, styrene oxide, phenyl glycidyl ether, 1,2-pentene oxide, tetramethyl ethylene oxide, trimethyl ethylene oxide, cyclohexene oxide, and mixtures thereof.
Claim 12
Dependent Claim
34 words
The pharmaceutical formulation of claim 1 wherein only one of R 1 , R 2 , R 3 , or R 4 in the esterified alkoxylated polyol carrier is a moiety other than hydrogen.
Claim 13
Dependent Claim
16 words
The pharmaceutical formulation of claim 1 wherein P in the esterified alkoxylated polyol carrier is glyceryl.
Claim 14
Dependent Claim
20 words
The pharmaceutical formulation of claim 1 wherein the sum of w+x+y+z in the esterified alkoxylated polyol carrier is about 3.
Claim 15
Dependent Claim
18 words
The pharmaceutical formulation of claim 1 wherein A in the esterified alkoxylated polyol carrier is an oxypropylene unit.
Claim 16
Dependent Claim
68 words
The pharmaceutical formulation of claim 1 wherein P is glyceryl, the sum of w+x+y+z is about 3, A is an oxypropylene unit, B is a C 13 -C 21 hydrocarbon group, the average value of [(m·z)+(n·y)] is in the range of from 0 to about 15, and only one of R 1 , R 2 , R 3 , or R 4 is a moiety other than hydrogen.
Claim 17
Dependent Claim
41 words
The pharmaceutical formulation of claim 1 wherein the sum of w+x+y+z is about 3, B is a C 13 -C 21 hydrocarbon group, and the average value of [(m z)+(n y)] is in the range of from 0 to about 15.
Claim 18
Dependent Claim
18 words
The pharmaceutical formulation of claim 1 wherein on average C: is from 0 to about 5 percent primary.
Claim 19
Dependent Claim
22 words
A method of administering a medication ingredient which comprises treating an animal or human subject with the pharmaceutical formulation of claim 1.
Claim 20
Dependent Claim
196 words
An improved pharmaceutical formulation comprising an effective amount of a medication ingredient in admixture with an esterified propoxylated glycerol carrier of formula ##STR20## wherein (a) P is a glyceryl radical, the sum of w+x+y+z is about 3, ##EQU7## is an average number less than about 0.15, z is an average number in the range of from about 2 to 3, A is an oxypropylene unit, the average value of [(m·z)+(n·y)] is in the range from 0 to about 15, B is a C 11 -C 21 hydrocarbon group, one only of R 1 , R 2 , R 3 , and R 4 is methyl with the other R groups being hydrogen, and C 2 is a carbon that on average is from 0 to about 5 percent primary; (b) said values of m, n, w, x, y, and z are selected to provide suitable pharmaceutical carrier properties; (c) said esterified propoxylated glycerol carrier is present in an amount sufficient to impart suitable body or coverage to said formulation; (d) said esterified propoxylated glycerol carrier is substantially dermally non-allergenic, non-irritating, non-digestible, and non-toxic; and (e) said pharmaceutical formulation is characterized by the absence of a foodstuff.
Claim 21
Dependent Claim
196 words
An improved pharmaceutical formulation comprising an effective amount of a medication ingredient in admixture with an esterified propoxylated glycerol carrier of formula ##STR20## wherein (a) P is a glyceryl radical, the sum of w+x+y+z is about 3, ##EQU7## is an average number less than about 0.15, z is an average number in the range of from about 2 to 3, A is an oxypropylene unit, the average value of [(m·z)+(n·y)] is in the range from 0 to about 15, B is a C 11 -C 21 hydrocarbon group, one only of R 1 , R 2 , R 3 , and R 4 is methyl with the other R groups being hydrogen, and C 2 is a carbon that on average is from 0 to about 5 percent primary; (b) said values of m, n, w, x, y, and z are selected to provide suitable pharmaceutical carrier properties; (c) said esterified propoxylated glycerol carrier is present in an amount sufficient to impart suitable body or coverage to said formulation; (d) said esterified propoxylated glycerol carrier is substantially dermally non-allergenic, non-irritating, non-digestible, and non-toxic; and (e) said pharmaceutical formulation is characterized by the absence of a foodstuff.
Claim 22
Dependent Claim
27 words
The pharmaceutical formulation of claim 19 wherein the esterified propoxylated glycerin carrier has an average value of ##EQU8## in the range of from 0 to about 0.05.
Claim 23
Dependent Claim
49 words
The pharmaceutical formulation of claim 19 wherein the ##STR21## group of the esterified propoxylated glycerin carrier is derived from a fatty acid selected from the group consisting of caprylic, capric, lauric, myristic, myristoleic, stearic, palmitic, palmitoleic, rincinoleic, linoleic, linolenic, elaeostearic, arachidic, behenic, erucic, oleic, heptadecanoic acid, and mixtures thereof.
Claim 24
Dependent Claim
21 words
A method of administering a medication ingredient which comprises treating an animal or human with the pharmaceutical formulation of claim 19.
Claim 25
Independent Claim
221 words
A method of rendering a medication ingredient suitable for administering to an animal or human subject having a lower gastrointestinal tract such that the medication ingredient is delivered to the lower gastrointestinal tract when said medication ingredient is ingested orally, said method comprising incororating the medication ingredient into a pharmaceutical formulation comprised of the medication ingredient and an effective amount of an esterified alkoxylated polyol carrier of formula ##STR22## wherein (a) P is an organic radcial derived from a polyol, the sum of w+x+y+z is from 2 to 8, ##EQU9## on an average number in the range of from 0 to about 0.15, z is an average number in the range of from about 2 to the sum of w+x+y+z, A is an oxyalkylene unit having at least 3 carbon atoms, B is a C 7 -C 23 hydrocarbon group, at least one of R 1 , R 2 , R 3 , or R 4 is a moiety other than hydrogen, and C 2 is a carbon that on average is from 0 to about 15 percent primary; (b) said values of m, n, w, x, y, and z are selected to provide suitable pharmaceutical carrier properties; and (c) said esterified alkoxylated polyol carrier is substantially non-digestible and non-toxic; wherein said pharmaceuticla formulation is characterized bythe absence of a foodstuff.
Claim 26
Independent Claim
221 words
A method of rendering a medication ingredient suitable for administering to an animal or human subject having a lower gastrointestinal tract such that the medication ingredient is delivered to the lower gastrointestinal tract when said medication ingredient is ingested orally, said method comprising incororating the medication ingredient into a pharmaceutical formulation comprised of the medication ingredient and an effective amount of an esterified alkoxylated polyol carrier of formula ##STR22## wherein (a) P is an organic radcial derived from a polyol, the sum of w+x+y+z is from 2 to 8, ##EQU9## on an average number in the range of from 0 to about 0.15, z is an average number in the range of from about 2 to the sum of w+x+y+z, A is an oxyalkylene unit having at least 3 carbon atoms, B is a C 7 -C 23 hydrocarbon group, at least one of R 1 , R 2 , R 3 , or R 4 is a moiety other than hydrogen, and C 2 is a carbon that on average is from 0 to about 15 percent primary; (b) said values of m, n, w, x, y, and z are selected to provide suitable pharmaceutical carrier properties; and (c) said esterified alkoxylated polyol carrier is substantially non-digestible and non-toxic; wherein said pharmaceuticla formulation is characterized bythe absence of a foodstuff.
Claim 27
Independent Claim
218 words
A method of rendering a medication ingredient suitable for administering to an animal or human subject having a lower gastrointestinal tract such that the medication ingredient is delivered to the lower gastrointestinal tract when said medication ingredient is ingested orally, said method comprising incorporating the medication ingredient into a pharmaceutical formulation comprised of the medication ingredient and an effective amount of an esterified propoxylated glycerol carrier of formula ##STR23## wherein (a) P is a glyceryl radicla, the sum of w+x+y+z is about 3, ##EQU10## is an average number less than about 0.15, z is an average number in the range of from about 2 to 3, A is an oxypropylene unit, the average value of [(m·z)+(n·y)] is in the range from 0 to about 15, B is a C 1 -C 21 hydrocarbon group, one only of R 1 , R 2 , R 3 , and R 4 is methyl with the other R groups being hydrogen, and C 2 is a carbon that on average is from 0 to about 5 percent primary; (b) said values of m, n, w, x, y, and z are selected to provide suitable pharmaceutical carrier properties; and (c) said esterified propoxylated glycerol carrier is substantially non-digestible and non-toxic; wherein said pharmaceutical formulation is characterized by the absence of a foodstuff.
Claim 28
Independent Claim
218 words
A method of rendering a medication ingredient suitable for administering to an animal or human subject having a lower gastrointestinal tract such that the medication ingredient is delivered to the lower gastrointestinal tract when said medication ingredient is ingested orally, said method comprising incorporating the medication ingredient into a pharmaceutical formulation comprised of the medication ingredient and an effective amount of an esterified propoxylated glycerol carrier of formula ##STR23## wherein (a) P is a glyceryl radicla, the sum of w+x+y+z is about 3, ##EQU10## is an average number less than about 0.15, z is an average number in the range of from about 2 to 3, A is an oxypropylene unit, the average value of [(m·z)+(n·y)] is in the range from 0 to about 15, B is a C 1 -C 21 hydrocarbon group, one only of R 1 , R 2 , R 3 , and R 4 is methyl with the other R groups being hydrogen, and C 2 is a carbon that on average is from 0 to about 5 percent primary; (b) said values of m, n, w, x, y, and z are selected to provide suitable pharmaceutical carrier properties; and (c) said esterified propoxylated glycerol carrier is substantially non-digestible and non-toxic; wherein said pharmaceutical formulation is characterized by the absence of a foodstuff.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1996-05-24 | 1996-11-23 | 1997-05-25 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2000-05-24 | 2000-11-23 | 2001-05-25 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2004-05-24 | 2004-11-23 | 2005-05-25 | $7700.00 | Window Closed / Lapsed |